Diazoxide
| PubChem = 3019 | DrugBank = APRD00914 | C = 8 | H = 7 | Cl = 1 | N = 2 | O = 2 | S = 1 | molecular_weight = 230.672 g/mol | bioavailability = | protein_bound = 90% | metabolism = Hepatic oxidation and sulfate conjugation | elimination_half-life = 21-45 hours | excretion = Renal | pregnancy_AU = C | pregnancy_US = C | legal_UK = POM | legal_US = Rx-only | routes_of_administration = Oral, intravenous }} Diazoxide is a potassium channel activator, which causes local relaxation in smooth muscle by increasing membrane permeability to potassium ions. This switches off voltage-gated calcium ion channels which inhibits the generation of an action potential. It is used as a vasodilator in the treatment of acute hypertension, and also to decrease the secretion of insulin in disease states such as insulinoma (a tumor producing insulin). | PubChem = 3019 | DrugBank = APRD00914 | C = 8 | H = 7 | Cl = 1 | N = 2 | O = 2 | S = 1 | molecular_weight = 230.672 g/mol | bioavailability = | protein_bound = 90% | metabolism = Hepatic oxidation and sulfate conjugation | elimination_half-life = 21-45 hours | excretion = Renal | pregnancy_AU = C | pregnancy_US = C | legal_UK = POM | legal_US = Rx-only | routes_of_administration = Oral, intravenous }} Diazoxide is a potassium channel activator, which causes local relaxation in smooth muscle by increasing membrane permeability to potassium ions. This switches off voltage-gated calcium ion channels which inhibits the generation of an action potential. It is used as a vasodilator in the treatment of acute hypertension, and also to decrease the secretion of insulin in disease states such as insulinoma (a tumor producing insulin). Referencess *Avshalumov, M. V., Chen, B. T., Koos, T., Tepper, J. M., & Rice, M. E. (2005). Endogenous Hydrogen Peroxide Regulates the Excitability of Midbrain Dopamine Neurons via ATP-Sensitive Potassium Channels: Journal of Neuroscience Vol 25(17) Apr 2005, 4222-4231. *Chi, X. X., Jiang, X., & Nicol, G. D. (2007). ATP-sensitive potassium currents reduce the PGE-sub-2-mediated enhancement of excitability in adult rat sensory neurons: Brain Research Vol 1145 May 2007, 28-40. *Cockhill, L. A., & Remick, R. A. (1987). Blood pressure effects of monoamine oxidase inhibitors: The highs and lows: The Canadian Journal of Psychiatry / La Revue canadienne de psychiatrie Vol 32(9) Dec 1987, 803-808. *Farkas, E., Institoris, A., Domoki, F., Mihaly, A., Luiten, P. G. M., & Bari, F. (2004). Diazoxide and dimethyl sulphoxide prevent cerebral hypoperfusion-related learning dysfunction and brain damage after carotid artery occlusion: Brain Research Vol 1008(2) May 2004, 252-260. *Hensley, I. E. (2000). Effects of diazoxide on NPY content in discrete brain nuclei of lean and obese zucker rats. Dissertation Abstracts International: Section B: The Sciences and Engineering. *Khalilzadeh, O., Anvari, M., Khalilzadeh, A., Sahebgharani, M., & Zarrindast, M. R. (2008). Involvement of amlodipine, diazoxide, and glibenclamide in development of morphine tolerance in mice: International Journal of Neuroscience Vol 118(4) Apr 2008, 503-518. *Kong, L.-L., & Yu, L.-C. (2006). It is AMPA receptor, not kainate receptor, that contributes to the NBQX-induced antinociception in the spinal cord of rats: Brain Research Vol 1100(1) Jul 2006, 73-77. *Niaki, S. E. A., Shafaroodi, H., Ghasemi, M., Shakiba, B., Fakhimi, A., & Dehpour, A. R. (2008). Mouth breathing increases the pentylenetetrazole-induced seizure threshold in mice: A role for ATP-sensitive potassium channels: Epilepsy & Behavior Vol 13(2) Aug 2008, 284-289. *Yang, Y., Liu, X., Long, Y., Wang, F., Ding, J.-H., Liu, S.-Y., et al. (2006). Activation of mitochondrial ATP-sensitive potassium channels improves rotenone-related motor and neurochemical alterations in rats: International Journal of Neuropsychopharmacology Vol 9(1) Feb 2006, 51-61. *Zarrindast, M. R., Jafari, M. R., Shafaghi, B., & Djahanguiri, B. (2004). Influence of potassium channel modulators on morphine state-dependent memory of passive avoidance: Behavioural Pharmacology Vol 15(2) Mar 2004, 103-110. Category:Sulfonamides Category:Vasodilators